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Assay Detail

CHEMBL4027225

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of PDE4 in human U937 cell lysates assessed as residual cAMP after 2.5 mins by LANCE assay
ChEMBL ↗
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases.
Carzaniga L, Amari G, Rizzi A, Capaldi C, De Fanti R, Ghidini E, Villetti G, Carnini C, Moretto N, Facchinetti F, Caruso P, Marchini G, Battipaglia L, Patacchini R, Cenacchi V, Volta R, Amadei F, Pappani A, Capacchi S, Bagnacani V, Delcanale M, Puccini P, Catinella S, Civelli M, Armani E.
J Med Chem (2017) 60 : 10026 -10046
PubMed 29200281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 10.08 10.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4099321 — — 1 10.85
CHEMBL4088655 — — 1 10.70
CHEMBL4079867 — — 1 10.68
CHEMBL4098825 — — 1 10.60
CHEMBL4093890 — — 1 10.59
CHEMBL4083617 — — 1 10.55
CHEMBL4104685 — — 1 10.51
CHEMBL4096951 — — 1 10.51
CHEMBL4068468 — — 1 10.49
CHEMBL4066195 — — 1 10.45
CHEMBL4093768 — — 1 10.42
CHEMBL4073209 — — 1 10.39
CHEMBL4063563 — — 1 10.37
CHEMBL4103930 — — 1 10.35
CHEMBL4104112 — — 1 10.33
CHEMBL4075951 — — 1 10.28
CHEMBL4091400 — — 1 10.27
CHEMBL4065344 — — 1 10.26
CHEMBL4093014 — — 1 10.25
CHEMBL4096178 — — 1 10.22
CHEMBL4060427 — — 1 10.21
CHEMBL3113937 — — 1 10.14
CHEMBL4069758 — — 1 10.03
CHEMBL4067195 — — 1 9.96
CHEMBL4080781 — — 1 9.75
CHEMBL4101624 — — 1 9.75
CHEMBL4086704 — — 1 9.74
CHEMBL4080587 — — 1 9.49
CHEMBL4065232 — — 1 9.49
CHEMBL4078123 — — 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4099321 — IC50 = 0.014 nM 10.85
CHEMBL4088655 — IC50 = 0.02 nM 10.70
CHEMBL4079867 — IC50 = 0.021 nM 10.68
CHEMBL4098825 — IC50 = 0.025 nM 10.60
CHEMBL4093890 — IC50 = 0.026 nM 10.59
CHEMBL4083617 — IC50 = 0.028 nM 10.55
CHEMBL4104685 — IC50 = 0.031 nM 10.51
CHEMBL4096951 — IC50 = 0.031 nM 10.51
CHEMBL4068468 — IC50 = 0.0324 nM 10.49
CHEMBL4066195 — IC50 = 0.0351 nM 10.45
CHEMBL4093768 — IC50 = 0.0378 nM 10.42
CHEMBL4073209 — IC50 = 0.041 nM 10.39
CHEMBL4063563 — IC50 = 0.043 nM 10.37
CHEMBL4103930 — IC50 = 0.0442 nM 10.35
CHEMBL4104112 — IC50 = 0.047 nM 10.33
CHEMBL4075951 — IC50 = 0.053 nM 10.28
CHEMBL4091400 — IC50 = 0.0533 nM 10.27
CHEMBL4065344 — IC50 = 0.055 nM 10.26
CHEMBL4093014 — IC50 = 0.056 nM 10.25
CHEMBL4096178 — IC50 = 0.06 nM 10.22
CHEMBL4060427 — IC50 = 0.061 nM 10.21
CHEMBL3113937 — IC50 = 0.072 nM 10.14
CHEMBL4069758 — IC50 = 0.094 nM 10.03
CHEMBL4067195 — IC50 = 0.109 nM 9.96
CHEMBL4080781 — IC50 = 0.176 nM 9.75
CHEMBL4101624 — IC50 = 0.176 nM 9.75
CHEMBL4086704 — IC50 = 0.183 nM 9.74
CHEMBL4080587 — IC50 = 0.32 nM 9.49
CHEMBL4065232 — IC50 = 0.323 nM 9.49
CHEMBL4078123 — IC50 = 0.5038 nM 9.30
CHEMBL4104817 — IC50 = 0.825 nM 9.08
CHEMBL4096370 — IC50 = 3.006 nM 8.52
CHEMBL4069111 — IC50 = 6.397 nM 8.19
CHEMBL4069299 — IC50 - — -